Biochem/physiol Actions

Reversible: yes

Primary Targetcaspase-3

Product does not compete with ATP.

Target K_i: 60 nM, 170 nM, against caspase-3 and caspase-7, respectively

Cell permeable: yes

General description

A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (K_i = 60 nM) and caspase-7 (K_i = 170 nM).

A potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (K_I(app) = 60 nM) and caspase-7 (K_I(app) = 170 nM). Inhibits caspase-9 to a lesser extent (K_i(app) = 3.1 µM). Has only a trivial effect (K_i(app) >25 mM) on the activities of caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8. Reported to inhibit apoptosis in camptothecin treated Jurkat cells (IC₅₀ ~50 µM). Also reported to inhibit apoptosis in chondrocytes (44% inhibition at 10 µM and 98% inhibition at 50 µM). Selectivity for caspases 3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Lee, D., et al. 2001. J. Med. Chem.44, 2015.Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sequence

5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin

Warning

Toxicity: Standard Handling (A)